Optically active thiazolo:isoindolinone derivs. - are antiviral agents, effective against diseases caused by DNA and by RNA viruses, and by retrovirus(es), esp. HIV

摘要

Optically active thiazoloisoindolinone derivs. of formula (I) and their tautomers are new. In (I), R is H or opt. branched, opt. satd. 1-7C alkyl which is opt. substd. with Ph, or is a Ph ring which is opt. mono- or poly-substd. with 1-4C alkyl, 1-4C alkoxy, OH, CF3, methylsulphonyl or halogen such as F, Cl or Br; R is in either (R) or (S) configuration; n is 0 or 1. (I) can be prepd. by sepg. known racemates of (I) into the enantiomers. USE/ADVANTAGE - (I) have excellent antiviral activity and can be used to treat viral and retroviral infections, e.g., those caused by DNA viruses such as Herpes simplex virus, Zytomegalia virus, Pamplloma virus, Varicella-Zoster virus or Epstain-Barr virus or by RNA (BNA - sic) viruses such as Toga virus, or esp. by retroviruses such as the onko viruses HTLV I and II and the lentiviruses Visna and HN 1 and 2. (I) are esp. useful in treating the clinical manifestations of retroviral HIV infections in humans, such as permanent generalised lymphadenopathy (PGL), advanced stages of ARC and the full blown AIDS. Suitable daily doses are 0.1-100 (esp. 0.2-80) mg/kg, pref. divided into 2-5 unit doses.